Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.

Abstract: Disclosed herein are mono-functional silylating compounds that may exhibit enhanced silylating capabilities. Also disclosed are method of synthesizing and using these compounds. Finally methods to determine effective silylation are also disclosed.

Abstract: The present application provides a process for the preparation of Bortezomib, its intermediates and process for crystalline forms of Bortezomib.

Abstract: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

Abstract: The present invention provides a compound represented by the formula (I): wherein ring A is void or a benzene ring optionally having substituent(s), R1 and R2 are each independently a phenyl group optionally having substituent(s), a cyclohexyl group and the like, R3 and R4 are each independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group and the like, and X is a residue represented by —OR5 or —NHR6 wherein R5 and R6 are a lower alkyl group optionally having substituent(s), an aralkyl group optionally having substituent(s) and the like, a asymmetric transition metal complex containing the compound as a ligand and a production method of optically active compound using the complex as an asymmetric catalyst.

Abstract: The present invention relates to an organic light-emitting diode comprising an anode An and a cathode Ka and a light-emitting layer E which is arranged between the anode An and the cathode Ka and comprises at least one carbene complex and if appropriate at least one further layer, where the light-emitting layer E and/or the at least one further layer comprises at least one compound selected from disilylcarbazoles, disilyldibenzofurans, disilyldibenzothiophenes, disilyldibenzophospholes, disilyldibenzothiophene S-oxides and disilyldibenzothiophene S,S-dioxides, to a light-emitting layer comprising at least one of the aforementioned compounds and at least one carbene complex, to the use of the aforementioned compounds as matrix material, hole/exciton blocker material, electron/exciton blocker material, hole injection material, electron injection material, hole conductor material and/or electron conductor material, and to a device selected from the group consisting of stationary visual display units, mobile visu

Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.

Abstract: The present invention provides a novel process for the preparation of the prulifloxacin intermediate, 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3] thiazeto[3,2-a]quinoline-3-carboxylic acid, thereby producing prulifloxacin and its pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates in lesser reaction time. Thus, for example, ethyl 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is reacted with boric acid in the presence of acetic anhydride and acetic acid to give a borane compound, which is then condensed with piperazine in the presence of acetonitrile and dimethylsulfoxide, followed by treatment with potassium hydroxide solution to give 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3] thiazeto [3,2-a]quinoline-3-carboxylic acid.

Abstract: Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.

Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

Abstract: The present invention relates to molecular probes of the formula (I) {L1-R1-L}n-A-CO—NH—R2-L2??(I) as defined herein that allow for the observation of the catalytic activity of a selected cathepsin in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.

Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: The present invention relates to a process for reversible hydrogen storage, to a material for reversible hydrogen storage and to the use of the material for reversible hydrogen storage.

Abstract: The present invention relates to pyrimidinylpyrazoles and their use as insecticides, and also to processes for their preparation and to compositions comprising such arylpyrazoles.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: The invention describes a composition comprising a) a naturally occurring or synthetic elastomer susceptible to oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation, b) a white reinforcing filler, and c) as coupling agent, at least one compound of the formula (I) wherein the general symbols are as defined in claim 1, or an oligomeric hydrolysis product of the compound of the formula (I).

Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH2)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: One aspect of the present invention relates to “boronium” ions that are stable, hydrophobic, room-temperature ionic liquids. In certain embodiments, ionic liquids of the instant invention are represented by the formula [XnBY4?n]+(n?1)(n?1)Z?1, wherein X refers to a Lewis base, Y refers to a substituent covalently bonded to boron, Z?1 is a charge diffuse anion, and x is 2, 3 or 4. In certain embodiments, the ionic liquids of the instant invention are of the general type [X2BY2]+1Tf2N?1, wherein each X is independently a tertiary amine, a N-alkylimidazole or a pyridine; and each B—X bond is a B—N bond.

Abstract: An organosilicon compound having an amino group is provided. This compound is represented by the following general formula (1): wherein R1 and R2 respectively represent an unsubstituted or substituted aliphatic monovalent hydrocarbon group containing 1 to 10 carbon atoms with the proviso that the R1 and R2 may together form a ring with the nitrogen atom to which they are bonded, and that R1 and R2 may contain a heteroatom; R3 and R4 independently represent an unsubstituted or substituted monovalent hydrocarbon group containing 1 to 10 carbon atoms; and n represents an integer of 0 to 2. Use of this compound enables production of a polymer product having excellent mechanical properties, high heat resistance, and high transparency. The solution of this compound is stable, and can be stored for a long time, and when used for a polymer modifying agent, it facilitates introduction of amino group and hydroxy group.

Abstract: There is disclosed nucleotides and nucleotide analogs having a protecting or “caging” group. There is further disclosed oligonucleotides and oligonucleotides analogs formed having a protecting or “caging” group. There is further disclosed a method for decaging the nucleotides and nucleotide analogs having a protecting or “caging” group and oligonucleotides and oligonucleotide analogs having a caging group.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: The present invention relates to new compounds of formula I wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

Abstract: Deoxyuridine derivatives of the formula where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis o treatment of parasitic diseases such as malaria

Abstract: Organosilicon compounds are represented by the following formula: wherein R is a hydrolyzable group, R? is an alkyl having 1 to 4 carbon atoms, A is an alkylene having 1 to 6 carbon atoms, X is O or S, Y is —NH— or S, L1 and L2 are C or N, Z and M are —NH—, O or S, R1 to R11 are H, alkyl having 1 to 6 carbon atoms, alkoxy or fluoroalkyl, or amino, m is 1 to 3, and n is 0 to 3. R1 and R2 or R2 and R3 may bonded together. R5 and R6 or R9 and R10 may directly bond together. R4 and R7 or R8 and R11 may form a ring skeleton. Their production processes, pressure-sensitive adhesive compositions, self-adhesive polarizers and LCDs are also disclosed.

Abstract: The invention relates to isothiourea derivatives of formula I: wherein R1 is a residue of one of the following structures: where the variables are as defined in the claims of the invention, as well as processes for production of these compounds.

Abstract: Disclosed are merocyanine derivatives which correspond to the formula (I), wherein L1, L2 and L3 independently of each other are hydrogen; or L1 and L3 may be linked together to form a carbocyclic ring; R3 and R4 independently of each other are CN; —COR5; —COOR5; —CONR5R6; C1-C22alkyl; C2-C22alkenyl; C2-C22alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C20aralkyl; C1-C20heteroalkyl; C3-C12cycloheteroalkyl; C3-C18heteroaralkyl; C6-C20 aryl; C1-C12alkylcarbonylamino-C6-C20aryl; C2-C12heteroaryl; or —X2—Sil2; n is a number from 1 to 4; the meaning of R1 and R2 depends on the definition of n. The compounds are useful as UV absorbers for cosmetic applications.

Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: The present invention relates to novel triazolopyrimidine derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity(I): wherein the substituents are as defined in claim 1. Characterizing feature is the cyclic silyl group.

Abstract: Active carrier that consists of a carrier base (1) and attached linkers containing activated linker functional groups. The active carrier contains two or more different activated linker functional groups. A process for the production of the active carrier that comprises a carrier base (1) and linkers containing activated linker functional groups. Steps of the process: a) binding of a linker containing one or more linker functional groups to the carrier base (1), through the carrier functional groups; and b) reacting the linker functional groups of the linkers bound to the carrier base in step a) with two or more different activating reagents simultaneously. Use of the active carrier, during which the surface of the active carrier is contacted with one or more solution of small molecules.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: The present invention relates to fluorinated aminoalkyl-4-oxo-3,4-dihydropyrido[3,4-d]pyrimidine derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: This invention relates to N and O-protected, optionally substituted ?-heteroaryl-?-alanine compounds of the structural Formula I, wherein each of the variables is as set forth in the specification, methods for producing and using the same.

Abstract: A compound of any of formulae (I) to (III) wherein at least one of Y and Z includes a Si atom, is of utility in therapy.

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.

Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.

Abstract: An optically active 2,3-bis(dialkylphosphino)pyrazine derivative represented by formula (1) is disclosed. The pyrazine derivative is preferably a quinoxaline derivative represented by formula (2). In formula (1) and (2), R1 is preferably a t-butyl or adamantyl group, and R2 is preferably a methyl group. wherein R1 is a substitutable straight chain or branched alkyl group having 2 to 10 carbon atoms; R2 is a substitutable straight chain or branched alkyl group having fewer carbon atoms than R1; and R3 and R4, which may be the same or different, are each a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, or R3 and R4 are taken together to form a saturated or unsaturated ring. wherein R1 and R2 are as defined above; and R5 is a monovalent substituent.

Abstract: A compound represented by the following general formula (I): {R1, R3, R6 and R8 are methyl groups and the like, R2 and R7 are cyano groups and the like, R4 and R5 are fluorine atoms and the like, and X is a group represented by the formula (A) [R11 is a monocarboxy-substituted C1-8 alkoxy group and the like, R12, R14 and R15 are hydrogen atoms and the like, and R13 is hydroxy group and the like], provided that the combination of the aforementioned substituents is such a combination that the compound represented by the formula (I) can be substantially non-fluorescent before reacting with peroxynitrite, and the compound represented by the formula (I) in which the group represented by the formula (A) is nitrated after reacting with peroxynitrite can be substantially highly fluorescent}, or a salt thereof, which is useful as a fluorescent probe for peroxynitrite measurement.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.

Abstract: ?-aminoalkoxysilanes wherein the ?-amino group is a tertiary amino group, and which also contains a further reactive group, display excellent reactivity of the alkoxy groups while remaining stable with respect to decomposition and byproduct formation, particularly through cleavage of the Si-C bond. The ?-aminosilanes are particularly useful for preparing alkoxysilyl-terminated prepolymers which exhibit high cure rates in the presence of moisture, and for functionalizing particles reactive therewith.

Abstract: The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron capture therapy (BNCT).

Abstract: A process is used for the preparation of 1,3,2-oxazaborolidine compounds. This process prepares compounds of formula (I) or (IA): in which: R1 is an alkyl or an aryl; and R2, R3, R4 and R5 are especially a hydrogen atom or an alkyl, wherein the following are reacted in two steps: a) a boric precursor compound with an acetal compound to give a boronate compound; and b) the boronate compound with an amino alcohol compound. This process avoids by-products and exhibits a very good stereospecificity.

Abstract: This invention provides a process for efficient production of folic acid derivatives suitable for forming conjugates of anticancer drug with folic acid. It discloses a process comprising a step of reacting 2-amino-protected pteroylimidazole with ?-lower alkyl glutamate; and a step of reacting the resulting product with an amino compound having a reactive group which is readily reactable with a functional group of the drug.

Abstract: The invention concerns compounds, oligomers, and polymers that contain: (I), (II), (III), or (IV) groups; where “-” indicates points of attachment.